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shows the synthesis of imidazole intermediates and The
2024-06-18
shows the synthesis of imidazole intermediates , , and . The key precursor keto aldehyde – was prepared in situ by SeO mediated oxidation of corresponding carbonyl compounds and or hydrolysis of dibromo ketone . Subsequent treatment with -Boc piperidine-4-carbaldehyde in the presence of aqueous
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The only psychostimulant treatment option in Turkey is
2024-06-18
The only psychostimulant treatment option in Turkey is methylphenidate (Çetin et al., 2015). It is broken down by carboxylase enzyme (CES1) (Sun et al., 2004). From the point of pharmacokinetics, it may be suggested that CES1 gene polymorphisms may be the key responsible factors in patients resistan
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Previous studies suggest that TGF contributes to the pathoge
2024-06-17
Previous studies suggest that TGF-β contributes to the pathogenesis of diabetic renal injury [47]. TGF-β stimulates matrix production and prevents matrix degradation, which leads to increase collagen deposition and glomerulosclerosis [48]. In the current study ABT702 significantly reduced renal coll
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G actin has a molecular
2024-06-17
G-actin has a molecular weight of 42 kD and dimensions about 55 × 55 × 35 Å3. It consists of 375 amino acids arranged into two individual domains (Alberts et al., 2014). A central cleft bisects the protein into two aforementioned domains which surround a deep cleft containing ATP or ADP and a tightl
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In terms of the ring B C
2024-06-17
In terms of the ring B C5′ position, while C5′-F (compound ) was tolerated, C5′-Me (compound ) and C5′-Cl (compound ) substitutions resulted in a loss in potency. However, the C5′-OMe substitution (compound ) resulted in a ∼3-fold increase in potency compared to . Modeling suggested a pseudo hydroge
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Most studies on d penicillamine induced MG
2024-06-17
Most studies on d-penicillamine-induced MG were performed before the discovery that some MG patients have anti-MuSK antibodies. After the identification of the present case, we retrospectively tested the stored frozen sera of ten earlier identified d-penicillamine MG patients with anti-AChR cystic f
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Whereas more research is needed to
2024-06-17
Whereas more research is needed to identify the precise mechanism by which FIN exerts its antidyskinetic effect, the (±)-J 113397 synthesis that it can negatively modulate dopaminergic transmission is also supported by our previous findings. Indeed, we have previously shown that FIN completely reve
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br The role of cytochrome b with cytochrome
2024-06-17
The role of cytochrome b5 with cytochrome P450 17α-hydroxylase/17,20-lyase Conclusion Acknowledgments LLM and RJR wish to thank the Australian Research Council and the National Health and Medical Research Council of Australia for funding. The problem One area of modern medicine that con
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Fencilli et al reported derivatives of PHA
2024-06-17
Fencilli et al. reported derivatives of PHA-680626 (15) which demonstrated strong anti-proliferative activity against large group of leukaemia cell lines including IM-resistant BAF3 cells expressing mutants like T315I, M351T and E255K. Decrease in Histone H3 phosphorylation led to induction of endo-
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Neuropathic animals display increased sensitivity to the ant
2024-06-17
Neuropathic animals display increased sensitivity to the anti-nociceptive effect of baclofen and whilst the number and affinity of GABAB Tubastatin A receptor in the dorsal horn are not altered (Smith et al., 1994; Zemoura et al., 2016), GABAB receptors subunits (B1 and B2) are both down-regulated i
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From an historical perspective ligands for GPCRs adrenaline
2024-06-17
From an historical perspective, ligands for GPCRs (adrenaline, serotonin, Tozasertib or morphine, to name a few) have been identified before their receptor counterparts, at a time when the concept of receptor itself was controversial [15]. Although many cognate receptors for endogenous ligands were
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Bioavailability has been defined as the amount of
2024-06-17
Bioavailability has been defined as the amount of a drug given by any route, other than intravenously, that reaches general circulation and is available at the site of action [86]. The low bioavailability observed with the initial intravaginal devices (16%) was attributed to the melting point of the
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Recently competitive inhibitors of arginase have been develo
2024-06-17
Recently, competitive inhibitors of arginase have been developed which have greater specificity for the enzyme. Initial development of these compounds involved determination of the crystal structure of arginase. Christianson and colleagues found that a binuclear manganese cluster was required for ca
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Previously we have detected the expression of APJ
2024-06-17
Previously, we have detected the expression of APJ receptor on stomach projecting EW-7197 in DMV, in addition, icv administration of apelin-13 induced a remarkable c-Fos activation in those cells which were previously marked by a retrograde neuronal tracer fast blue (Birsen et al., 2016). Moreover,
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Introduction Heterotrimeric G proteins mediate signal transd
2024-06-17
Introduction Heterotrimeric Gαβγ proteins mediate signal transduction through seven-transmembrane domain receptors. In response to neurotransmitters or hormones, activated receptors bind GTP via the Gα subunit leading to the dissociation of Gα from the Gβγ dimer. G proteins regulate the levels of s
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